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Assay Detail

CHEMBL5316640

Review assay metadata, readout intent, target linkage, and publication context from the same page.

Binding
Displacement of [125I]alpha-Bungarotoxin from human alpha7 nAChR expressed in human SH-SY5Y cell membrane assessed as inhibition constant by direct gamma counting method
33
Total Activities
33
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Homo sapiens
Cell Type SH-SY5Y
Subcellular Membrane
Confidence 9 — Direct single protein target
Curated By Autocuration

Target

Neuronal acetylcholine receptor subunit alpha-7 (CHEMBL2492)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Subnanomolar Affinity and Selective Antagonism at α7 Nicotinic Receptor by Combined Modifications of 2-Triethylammonium Ethyl Ether of 4-Stilbenol (MG624).
Bavo F, Pallavicini M, Pucci S, Appiani R, Giraudo A, Oh H, Kneisley DL, Eaton B, Lucero L, Gotti C, Clementi F, Whiteaker P, Bolchi C.
J Med Chem (2023) 66 : 306 -332
PubMed 36526469 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 33 6.44 9.00

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL5393773 1 9.00
CHEMBL5417751 1 7.72
CHEMBL5178473 1 7.64
CHEMBL5433741 1 7.47
CHEMBL5423336 1 7.09
CHEMBL1257065 STILONIUM IODIDE 2.0 1 6.98
CHEMBL5435415 1 6.89
CHEMBL5416962 1 6.78
CHEMBL5409285 1 6.74
CHEMBL4287656 1 6.72
CHEMBL5403618 1 6.62
CHEMBL5436520 1 6.60
CHEMBL5435510 1 6.54
CHEMBL5407945 1 6.47
CHEMBL5395819 1 6.45
CHEMBL5400651 1 6.35
CHEMBL5396300 1 6.28
CHEMBL5408237 1 6.28
CHEMBL5418191 1 6.24
CHEMBL5415738 1 6.21
CHEMBL5415788 1 6.18
CHEMBL5428774 1 6.14
CHEMBL5396579 1 6.06
CHEMBL5415255 1 6.00
CHEMBL5412463 1 6.00
CHEMBL5425014 1 5.99
CHEMBL5415576 1 5.88
CHEMBL5416363 1 5.87
CHEMBL5406306 1 5.82
CHEMBL5399641 1 5.78

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL5393773 Ki = 1.0 nM 9.00
CHEMBL5417751 Ki = 19.0 nM 7.72
CHEMBL5178473 Ki = 23.0 nM 7.64
CHEMBL5433741 Ki = 34.0 nM 7.47
CHEMBL5423336 Ki = 81.0 nM 7.09
CHEMBL1257065 STILONIUM IODIDE Ki = 104.0 nM 6.98
CHEMBL5435415 Ki = 129.0 nM 6.89
CHEMBL5416962 Ki = 166.0 nM 6.78
CHEMBL5409285 Ki = 184.0 nM 6.74
CHEMBL4287656 Ki = 189.0 nM 6.72
CHEMBL5403618 Ki = 242.0 nM 6.62
CHEMBL5436520 Ki = 250.0 nM 6.60
CHEMBL5435510 Ki = 285.0 nM 6.54
CHEMBL5407945 Ki = 342.0 nM 6.47
CHEMBL5395819 Ki = 353.0 nM 6.45
CHEMBL5400651 Ki = 450.0 nM 6.35
CHEMBL5396300 Ki = 525.0 nM 6.28
CHEMBL5408237 Ki = 526.0 nM 6.28
CHEMBL5418191 Ki = 573.0 nM 6.24
CHEMBL5415738 Ki = 621.0 nM 6.21
CHEMBL5415788 Ki = 664.0 nM 6.18
CHEMBL5428774 Ki = 723.0 nM 6.14
CHEMBL5396579 Ki = 862.0 nM 6.06
CHEMBL5415255 Ki = 1010.0 nM 6.00
CHEMBL5412463 Ki = 1004.0 nM 6.00
CHEMBL5425014 Ki = 1036.0 nM 5.99
CHEMBL5415576 Ki = 1334.0 nM 5.88
CHEMBL5416363 Ki = 1347.0 nM 5.87
CHEMBL5406306 Ki = 1525.0 nM 5.82
CHEMBL5399641 Ki = 1646.0 nM 5.78
CHEMBL5432840 Ki = 2600.0 nM 5.58
CHEMBL5415482 Ki = 3107.0 nM 5.51
CHEMBL5396724 Ki = 27000.0 nM 4.57